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Search for "regulation" in Full Text gives 132 result(s) in Beilstein Journal of Organic Chemistry.

Small anion-assisted electrochemical potential splitting in a new series of bistriarylamine derivatives: organic mixed valency across a urea bridge and zwitterionization

  • Keishiro Tahara,
  • Tetsufumi Nakakita,
  • Alyona A. Starikova,
  • Takashi Ikeda,
  • Masaaki Abe and
  • Jun-ichi Kikuchi

Beilstein J. Org. Chem. 2019, 15, 2277–2286, doi:10.3762/bjoc.15.220

Graphical Abstract
  • )•+ radical cations having dithienylethene bridges [21][22]. This was achieved by a regulation of the π-conjugation length through photoinduced formation/dissociation of σ bonds in the bridge, which was accomplished with changeovers from a localized system (class I) to a moderately delocalized one (class II
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Published 24 Sep 2019

A review of the total syntheses of triptolide

  • Xiang Zhang,
  • Zaozao Xiao and
  • Hongtao Xu

Beilstein J. Org. Chem. 2019, 15, 1984–1995, doi:10.3762/bjoc.15.194

Graphical Abstract
  • pathways involved in the regulation of reactive oxygen species (ROS) and/or nitric oxide (NO) [9], histone methyltransferase [10], HSP70 [11], Jak2, Bcl-2/Bax [12], caspase 8 [13], NF-κB [14], X-linked inhibitor of apoptosis protein (XIAP) [15], MAPK, PI3K [16], and MPK1, ERK-1/2, and JNK-1/2 [17]. The
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Published 22 Aug 2019

Host–guest interactions in nor-seco-cucurbit[10]uril: novel guest-dependent molecular recognition and stereoisomerism

  • Xiaodong Zhang,
  • Wei Wu,
  • Zhu Tao and
  • Xin-Long Ni

Beilstein J. Org. Chem. 2019, 15, 1705–1711, doi:10.3762/bjoc.15.166

Graphical Abstract
  • importance in the study of enzymatic catalysis and allosteric regulation of cell signaling, as well as in the design of efficient drugs that utilize host–guest interactions [1]. Cucurbit[n]urils (Q[n]s or CB[n]s) [2][3] having been viewed to have high potential use in host–guest chemistry in aqueous solution
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Published 19 Jul 2019

Molecular basis for the plasticity of aromatic prenyltransferases in hapalindole biosynthesis

  • Takayoshi Awakawa and
  • Ikuro Abe

Beilstein J. Org. Chem. 2019, 15, 1545–1551, doi:10.3762/bjoc.15.157

Graphical Abstract
  • beneficial bioactivities, exemplified by 12-epi-hapalindole E isonitrile, which exhibits antibacterial, antifungal, and antimycobacterial activities [16], and ambiguine I, which induces apoptosis and cell-cycle arrest through the inhibition of an NF-κB-related regulation pathway [17]. To investigate their
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Published 11 Jul 2019

Selective detection of DABCO using a supramolecular interconversion as fluorescence reporter

  • Indrajit Paul,
  • Debabrata Samanta,
  • Sudhakar Gaikwad and
  • Michael Schmittel

Beilstein J. Org. Chem. 2019, 15, 1371–1378, doi:10.3762/bjoc.15.137

Graphical Abstract
  • [14][15][16][17] and oscillators [18]. Recent work from our group [19] has strived for combining metallosupramolecular transformation(s) [20] with the creation of emergent functions, for instance by presenting three-state catalytic machinery with up and down regulation [21] or for networking catalytic
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Published 21 Jun 2019

Mechanistic investigations on multiproduct β-himachalene synthase from Cryptosporangium arvum

  • Jan Rinkel and
  • Jeroen S. Dickschat

Beilstein J. Org. Chem. 2019, 15, 1008–1019, doi:10.3762/bjoc.15.99

Graphical Abstract
  • a single enzyme that can produce a beneficial mixture, the advantage for the producing organism is even higher. Therefore, selectivity is not in every case the highest goal for evolution. An enzyme class, which is highly prone to a regulation of product selectivity for the production of either one
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Published 02 May 2019

Synthesis of acylglycerol derivatives by mechanochemistry

  • Karen J. Ardila-Fierro,
  • Andrij Pich,
  • Marc Spehr,
  • José G. Hernández and
  • Carsten Bolm

Beilstein J. Org. Chem. 2019, 15, 811–817, doi:10.3762/bjoc.15.78

Graphical Abstract
  • yields up to 91% (Scheme 4). Particularly interesting was the formation of DAG (18:0/20:4) 5d, an important lipidic backbone present in the biologically relevant phosphatidylinositol 4,5-bisphosphate (PIP2) [22]. In fact, diacylglycerols have proven to play vital roles in regulation of lipid bilayer and
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Published 29 Mar 2019

Azologization of serotonin 5-HT3 receptor antagonists

  • Karin Rustler,
  • Galyna Maleeva,
  • Piotr Bregestovski and
  • Burkhard König

Beilstein J. Org. Chem. 2019, 15, 780–788, doi:10.3762/bjoc.15.74

Graphical Abstract
  • -HT3A and 5-HT3B receptor subunits [22][23][24]. 5-HT3 receptors are highly expressed in the brainstem, especially in areas involved in the vomiting reflex and in the dorsal horn of the spinal cord [25]. These receptors are also expressed presynaptically providing regulation of the neurotransmitters
  • improve prospective antagonists and obtain a systematic tool for receptor investigation, spatial and temporal restriction of ligand binding and concomitant activity regulation is desirable. Fuelled by light, the growing field of photopharmacology provides a noninvasive method to trigger a drug’s
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Published 25 Mar 2019

Design and synthesis of multivalent α-1,2-trimannose-linked bioerodible microparticles for applications in immune response studies of Leishmania major infection

  • Chelsea L. Rintelmann,
  • Tara Grinnage-Pulley,
  • Kathleen Ross,
  • Daniel E. K. Kabotso,
  • Angela Toepp,
  • Anne Cowell,
  • Christine Petersen,
  • Balaji Narasimhan and
  • Nicola Pohl

Beilstein J. Org. Chem. 2019, 15, 623–632, doi:10.3762/bjoc.15.58

Graphical Abstract
  • administration to L. major infected mice (Figure 4). Results and Discussion To further probe the biological mechanisms responsible for L. major immune regulation, a new adjuvant-like pathogen-associated molecular probe was designed to promote pathogen recognition receptor (PRR)-mediated internalization and slow
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Published 11 Mar 2019

Synthesis and biological activity of methylated derivatives of the Pseudomonas metabolites HHQ, HQNO and PQS

  • Sven Thierbach,
  • Max Wienhold,
  • Susanne Fetzner and
  • Ulrich Hennecke

Beilstein J. Org. Chem. 2019, 15, 187–193, doi:10.3762/bjoc.15.18

Graphical Abstract
  • (HHQ, 1) are important signaling molecules involved in quorum sensing and as such play an important role in virulence regulation [3][10][11][12]. Another metabolite from the AQ biosynthesis pathway of P. aeruginosa is 2-heptyl-1-hydroxy-4(1H)-quinolone (generally referred to as 2-heptyl-4
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Published 21 Jan 2019

Repurposing the anticancer drug cisplatin with the aim of developing novel Pseudomonas aeruginosa infection control agents

  • Mingjun Yuan,
  • Song Lin Chua,
  • Yang Liu,
  • Daniela I. Drautz-Moses,
  • Joey Kuok Hoong Yam,
  • Thet Tun Aung,
  • Roger W. Beuerman,
  • May Margarette Santillan Salido,
  • Stephan C. Schuster,
  • Choon-Hong Tan,
  • Michael Givskov,
  • Liang Yang and
  • Thomas E. Nielsen

Beilstein J. Org. Chem. 2018, 14, 3059–3069, doi:10.3762/bjoc.14.284

Graphical Abstract
  • ). Together with the transcriptome profiling, this result confirmed that cisplatin was able to interact with the P. aeruginosa DNA, resulting in up-regulation of stress response genes. This mechanism was also similar to the mechanism of action by another DNA crosslinker, mitomycin C which kills bacterial
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Published 14 Dec 2018

Green synthesis of new chiral 1-(arylamino)imidazo[2,1-a]isoindole-2,5-diones from the corresponding α-amino acid arylhydrazides in aqueous medium

  • Nadia Bouzayani,
  • Jamil Kraїem,
  • Sylvain Marque,
  • Yakdhane Kacem,
  • Abel Carlin-Sinclair,
  • Jérôme Marrot and
  • Béchir Ben Hassine

Beilstein J. Org. Chem. 2018, 14, 2923–2930, doi:10.3762/bjoc.14.271

Graphical Abstract
  • have been known as an important herbicides for bud growth inhibition [2][3][4][5][6] and plant growth regulation [7][8][9][10][11]. Several research groups have turned to the synthesis of these structural analogues (Figure 1) [12]. For example, the stereoselective synthesis of chiral 1H-imidazo[2,1-a
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Published 26 Nov 2018

Protein–protein interactions in bacteria: a promising and challenging avenue towards the discovery of new antibiotics

  • Laura Carro

Beilstein J. Org. Chem. 2018, 14, 2881–2896, doi:10.3762/bjoc.14.267

Graphical Abstract
  • regulation of gene expression, DNA replication, signal transduction, virulence, etc. and therefore represent potential fruitful targets for antibacterial drug discovery. Recently, scientific efforts have helped towards the understanding and the deciphering of the protein-interaction networks (PINs) that
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Published 21 Nov 2018

Synthesis and biological evaluation of 1,2-disubstituted 4-quinolone analogues of Pseudonocardia sp. natural products

  • Stephen M. Geddis,
  • Teodora Coroama,
  • Suzanne Forrest,
  • James T. Hodgkinson,
  • Martin Welch and
  • David R. Spring

Beilstein J. Org. Chem. 2018, 14, 2680–2688, doi:10.3762/bjoc.14.245

Graphical Abstract
  • -position [14][15]. As a measure of modulation of QS in P. aeruginosa, it was desired to measure the amount of pyocyanin produced by bacterial cultures after treatment with the compounds. This virulence factor is known to be under the regulation of PQS signalling system, and is capable of disrupting many
  • work in each case, and suggests that it may be possible to attain selective therapeutic treatment of a specific species. Furthermore, the saturated series of analogues were demonstrated to inhibit the production of pyocyanin by P. aeruginosa, a virulence factor known to be under QS regulation
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Published 19 Oct 2018

Non-native autoinducer analogs capable of modulating the SdiA quorum sensing receptor in Salmonella enterica serovar Typhimurium

  • Matthew J. Styles and
  • Helen E. Blackwell

Beilstein J. Org. Chem. 2018, 14, 2651–2664, doi:10.3762/bjoc.14.243

Graphical Abstract
  • has lagged behind [4]. In recent years, non-bacteriocidal approaches have emerged as a new therapeutic strategy to treat infection with potentially a lesser propensity for resistance development and spread [4][5][6]. Interfering with the regulation of virulence phenotypes represents one such approach
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Published 17 Oct 2018

Targeting the Pseudomonas quinolone signal quorum sensing system for the discovery of novel anti-infective pathoblockers

  • Christian Schütz and
  • Martin Empting

Beilstein J. Org. Chem. 2018, 14, 2627–2645, doi:10.3762/bjoc.14.241

Graphical Abstract
  • and other pathogenicity traits to overwhelm and colonise the host in the infection process [5] and pqs QS plays a crucial role in the regulation of many of those. It is astonishing, that expression of 182 genes is altered in response to exogenous PQS [33]. Evidence has been gathered, that these
  • response. In terms of pathogenicity traits, they are involved in the regulation of genes encoding for enzymes responsible for phenazine biosynthesis (pyocyanin production), hydrogen cyanide synthesis, Lectins LecA and LecB and additional genes involved in biofilm formation, enzymes for rhamnolipid
  • synthesis, a Resistance-Nodulation-Cell division (RND) efflux pump encoded by mexGHI-opmD operon, components of Type 3 and Type 6 secretion as well as the exotoxin ExoS, and siderophore synthases [33]. In addition to virulence regulation, some remarkable secondary effects have been attributed to the PQS
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Published 15 Oct 2018

Impact of Pseudomonas aeruginosa quorum sensing signaling molecules on adhesion and inflammatory markers in endothelial cells

  • Carmen Curutiu,
  • Florin Iordache,
  • Veronica Lazar,
  • Aurelia Magdalena Pisoschi,
  • Aneta Pop,
  • Mariana Carmen Chifiriuc and
  • Alina Maria Hoban

Beilstein J. Org. Chem. 2018, 14, 2580–2588, doi:10.3762/bjoc.14.235

Graphical Abstract
  • and blood dissemination of the infection [3]. The regulation of the virulence factors expression is coordinated by quorum sensing (QS), an intercellular communication system based on cell density dependent molecules with autoinductory properties that play a pivotal role in the pathogenesis of various
  • therapeutic strategies against P. aeruginosa infections, which are very difficult to treat. The vascular endothelium is crucial for cell and tissue homeostasis and regulation of inflammatory response. The loss of its integrity causes plasma, proteins and cells to build up in the interstitial space, resulting
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Published 05 Oct 2018

Comparative cell biological study of in vitro antitumor and antimetastatic activity on melanoma cells of GnRH-III-containing conjugates modified with short-chain fatty acids

  • Eszter Lajkó,
  • Sarah Spring,
  • Rózsa Hegedüs,
  • Beáta Biri-Kovács,
  • Sven Ingebrandt,
  • Gábor Mező and
  • László Kőhidai

Beilstein J. Org. Chem. 2018, 14, 2495–2509, doi:10.3762/bjoc.14.226

Graphical Abstract
  • the regulation of gonadal steroidogenesis and gametogenesis by integrating the nervous and endocrine system in the pituitary gland [4]. Regarding the targeted chemotherapy, it is highly advantageous that several native GnRH analogs, including the two human isoforms (GnRH-I and GnRH-II), and their
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Published 26 Sep 2018

Bioinspired cobalt cubanes with tunable redox potentials for photocatalytic water oxidation and CO2 reduction

  • Zhishan Luo,
  • Yidong Hou,
  • Jinshui Zhang,
  • Sibo Wang and
  • Xinchen Wang

Beilstein J. Org. Chem. 2018, 14, 2331–2339, doi:10.3762/bjoc.14.208

Graphical Abstract
  • reactions. The “Co4O4” cubane complex Co4O4(CO2Me)4(RNC5H4)4 (R = CN, Br, H, Me, OMe), serves as a molecular catalyst for the efficient and stable photocatalytic water oxidation and CO2 reduction. A comprehensive structure–function analysis emerged herein, highlights the regulation of electronic
  • redox potentials reflect a dependence on the electronic properties of the ligand. This again underlines, that the ligands are playing a significant role in the regulation of the redox properties of the 1-R complexes. To further estimate the impact of ligand substitution, the complexes were analyzed by
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Published 05 Sep 2018

Rational design of boron-dipyrromethene (BODIPY) reporter dyes for cucurbit[7]uril

  • Mohammad A. Alnajjar,
  • Jürgen Bartelmeß,
  • Robert Hein,
  • Pichandi Ashokkumar,
  • Mohamed Nilam,
  • Werner M. Nau,
  • Knut Rurack and
  • Andreas Hennig

Beilstein J. Org. Chem. 2018, 14, 1961–1971, doi:10.3762/bjoc.14.171

Graphical Abstract
  • combination of properties has enabled numerous applications in the life sciences, for example, for protein binding [5][6], stabilization [7], immobilisation [8], isolation [9], self-assembly [10][11], and regulation [12], or for drug solubilisation and delivery [13][14][15]. The combination of CBs with
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Published 30 Jul 2018

An overview of recent advances in duplex DNA recognition by small molecules

  • Sayantan Bhaduri,
  • Nihar Ranjan and
  • Dev P. Arya

Beilstein J. Org. Chem. 2018, 14, 1051–1086, doi:10.3762/bjoc.14.93

Graphical Abstract
  • structural analogs of distamycin, netropsin and thiazotropsins were developed to test their DNA binding affinity, sequence specificity and cytotoxicity, thereby eventually developing a general approach for the regulation of gene expression by DNA binding small molecules. However, all these analogs do not
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Published 16 May 2018

Nanoreactors for green catalysis

  • M. Teresa De Martino,
  • Loai K. E. A. Abdelmohsen,
  • Floris P. J. T. Rutjes and
  • Jan C. M. van Hest

Beilstein J. Org. Chem. 2018, 14, 716–733, doi:10.3762/bjoc.14.61

Graphical Abstract
  • individually incorporated into the polymersomes and mixed together in solution; in both of the cases the final product formation was monitored by UV–vis spectroscopy. The control over the pH allowed the regulation of the enzymatic cascade (no product was observed at pH 8 in both of the reactive systems), as
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Published 29 Mar 2018

Stimuli-responsive oligonucleotides in prodrug-based approaches for gene silencing

  • Françoise Debart,
  • Christelle Dupouy and
  • Jean-Jacques Vasseur

Beilstein J. Org. Chem. 2018, 14, 436–469, doi:10.3762/bjoc.14.32

Graphical Abstract
  • such as gene regulation is to circumvent the poor chemical stability of nucleic acids in biological media due to their low resistance to nucleases and to overcome their low cell uptake due to their polyanionic nature. In the present review, we aimed to identify various ON prodrugs that are responsive
  • in vitro as in HeLa cells. Modifications at the nucleobase For selected reviews on this topic, see [79][80]. From all possible photoresponsive modifications introduced into ONs, modifications of the nucleobases are the most widely used for the regulation of gene expression under light activation. For
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Published 19 Feb 2018

Aminosugar-based immunomodulator lipid A: synthetic approaches

  • Alla Zamyatina

Beilstein J. Org. Chem. 2018, 14, 25–53, doi:10.3762/bjoc.14.3

Graphical Abstract
  • ). Application of natural or synthetic TLR4 antagonists represents one of the most effective approaches for down-regulation of the TLR4-mediated signaling. So far, several lipid A variants which can block the LPS-binding site on human (h)MD-2 have been identified: tetraacylated lipid IVa [47] and a non
  • -pathogenic lipid A from R. sphaeroides [22][48], which served as structural basis for the synthetic antisepsis drug candidate eritoran [49][50]. Inadequate regulation of the TLR4-mediated signaling was recognized as crucial factor in the pathogenesis of chronic inflammatory, autoimmune and infectious
  • diseases [51][52][53]. A number of studies also suggested a possible implication of TLR4 in cardiovascular disorders [54] and Alzheimer desease – associated pathology [55]. Therapeutic down-regulation of the TLR4 signaling is believed to be beneficial for treatment of numerous chronic and acute
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Published 04 Jan 2018

A concise flow synthesis of indole-3-carboxylic ester and its derivatisation to an auxin mimic

  • Marcus Baumann,
  • Ian R. Baxendale and
  • Fabien Deplante

Beilstein J. Org. Chem. 2017, 13, 2549–2560, doi:10.3762/bjoc.13.251

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  • , this created a convenient staging point to generate intermediate holding batches of material for subsequent on demand processing. Overall we envisage this laboratory scale design to offer several opportunities for further development enabling quick up regulation of production in the future
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Published 29 Nov 2017
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